Binding Site Information of Target
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T94201 | Target Info | |||
| Target Name | SRSF protein kinase 1 (SRPK1) | ||||
| Synonyms | Serine/arginine-rich protein-specific kinase 1; SR-protein-specific kinase 1; SFRS protein kinase 1 | ||||
| Target Type | Preclinical Target | ||||
| Gene Name | SRPK1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: L-alanine | Ligand Info | |||||
| Structure Description | Crystal structure of SR protein kinase 1 complexed to its substrate ASF/SF2 | PDB:3BEG | ||||
| Method | X-ray diffraction | Resolution | 2.90 Å | Mutation | No | [1] |
| PDB Sequence |
LVKIGDLFNG
78 RYHVIRKLGW88 GHFSTVWLSW98 DIQGKKFVAM108 KVVKSAEHYT118 ETALDEIRLL 128 KSVRNSDPND138 PNREMVVQLL148 DDFKISGVNG158 THICMVFEVL168 GHHLLKWIIK 178 SNYQGLPLPC188 VKKIIQQVLQ198 GLDYLHTKCR208 IIHTDIKPEN218 ILLSVNEQYI 228 RRLAAEAAGN477 FLVNPLEPKN487 AEKLKVKIAD497 LGNACWVHKH507 FTEDIQTRQY 517 RSLEVLIGSG527 YNTPADIWST537 ACMAFELATG547 DYLFEPHSGE557 EYTRDEDHIA 567 LIIELLGKVP577 RKLIVAGKYS587 KEFFTKKGDL597 KHITKLKPWG607 LFEVLVEKYE 617 WSQEEAAGFT627 DFLLPMLELI637 PEKRATAAEC647 LRHPWLNS
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| Ligand Name: Alectinib | Ligand Info | |||||
| Structure Description | SRPK1 in complex with Alectinib | PDB:5XV7 | ||||
| Method | X-ray diffraction | Resolution | 2.32 Å | Mutation | No | [2] |
| PDB Sequence |
YHLVKIGDLF
76 NGRYHVIRKL86 GWGHFSTVWL96 SWDIQGKKFV106 AMKVVKSAEH116 YTETALDEIR 126 LLKSVRNSDP136 NDPNREMVVQ146 LLDDFKISGV156 NGTHIVMVFE166 VLGHHLLKWI 176 IKSNYQGLPL186 PCVKKIIQQV196 LQGLDYLHTK206 CRIIHTDIKP216 ENILLSVNEQ 226 YIRRLAAEAT236 ENFLVNPLEP485 KNAEKLKVKI495 ADLGNACWVH505 KHFTEDIQTR 515 QYRSLEVLIG525 SGYNTPADIW535 STACMAFELA545 TGDYLFEPHS555 GEEYTRDEDH 565 IALIIELLGK575 VPRKLIVAGK585 YSKEFFTKKG595 DLKHITKLKP605 WGLFEVLVEK 615 YEWSQEEAAG625 FTDFLLPMLE635 LIPEKRATAA645 ECLRHPWLNS655 |
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ARG84
3.653
LEU86
3.093
GLY87
3.903
VAL94
3.870
LEU96
4.931
ALA107
3.678
LYS109
4.886
GLU124
4.658
VAL145
4.135
PHE165
3.320
GLU166
4.081
VAL167
3.549
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| Ligand Name: SPHINX31 | Ligand Info | |||||
| Structure Description | Crystal structure of SRPK1 in complex with SPHINX31 | PDB:5MY8 | ||||
| Method | X-ray diffraction | Resolution | 1.70 Å | Mutation | No | [3] |
| PDB Sequence |
KGGYHLVKIG
73 DLFNGRYHVI83 RKLGWGHFST93 VWLSWDIQGK103 KFVAMKVVKS113 AEHYTETALD 123 EIRLLKSVRN133 SDPNDPNREM143 VVQLLDDFKI153 SGVNGTHICM163 VFEVLGHHLL 173 KWIIKSNYQG183 LPLPCVKKII193 QQVLQGLDYL203 HTKCRIIHTD213 IKPENILLSV 223 NEQYIRRLAA233 EATEWQRFLV480 NPLEPKNAEK490 LKVKIADLGN500 ACWVHKHFTE 510 DIQTRQYRSL520 EVLIGSGYNT530 PADIWSTACM540 AFELATGDYL550 FEPHSGEEYT 560 RDEDHIALII570 ELLGKVPRKL580 IVAGKYSKEF590 FTKKGDLKHI600 TKLKPWGLFE 610 VLVEKYEWSQ620 EEAAGFTDFL630 LPMLELIPEK640 RATAAECLRH650 PWLNS |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .RXZ or .RXZ2 or .RXZ3 or :3RXZ;style chemicals stick;color identity;select .A:86 or .A:87 or .A:88 or .A:89 or .A:92 or .A:93 or .A:94 or .A:107 or .A:109 or .A:124 or .A:145 or .A:165 or .A:166 or .A:167 or .A:168 or .A:169 or .A:170 or .A:171 or .A:220 or .A:223 or .A:227 or .A:228 or .A:231 or .A:496 or .A:497; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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LEU86
3.675
GLY87
4.120
TRP88
3.482
GLY89
3.562
SER92
3.146
THR93
4.869
VAL94
3.667
ALA107
3.647
LYS109
3.209
GLU124
4.236
VAL145
4.018
PHE165
3.525
GLU166
3.192
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| Ligand Name: SRPIN-340 | Ligand Info | |||||
| Structure Description | Crystal structure of human SRPK1 complexed to an inhibitor SRPIN340 | PDB:4WUA | ||||
| Method | X-ray diffraction | Resolution | 2.00 Å | Mutation | No | [4] |
| PDB Sequence |
LVKIGDLFNG
78 RYHVIRKLGW88 GHFSTVWLSW98 DIQGKKFVAM108 KVVKSAEHYT118 ETALDEIRLL 128 KSVRNSDPND138 PNREMVVQLL148 DDFKISGVNG158 THICMVFEVL168 GHHLLKWIIK 178 SNYQGLPLPC188 VKKIIQQVLQ198 GLDYLHTKCR208 IIHTDIKPEN218 ILLSVNEQYI 228 RRLAAEATVN481 PLEPKNAEKL491 KVKIADLGNA501 CWVHKHFTED511 IQTRQYRSLE 521 VLIGSGYNTP531 ADIWSTACMA541 FELATGDYLF551 EPHSGEEYTR561 DEDHIALIIE 571 LLGKVPRKLI581 VAGKYSKEFF591 TKKGDLKHIT601 KLKPWGLFEV611 LVEKYEWSQE 621 EAAGFTDFLL631 PMLELIPEKR641 ATAAECLRHP651 WLNS
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .3UL or .3UL2 or .3UL3 or :33UL;style chemicals stick;color identity;select .A:86 or .A:87 or .A:94 or .A:96 or .A:107 or .A:145 or .A:165 or .A:166 or .A:167 or .A:168 or .A:169 or .A:170 or .A:171 or .A:220 or .A:223 or .A:227 or .A:228 or .A:231 or .A:496 or .A:497; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: adenosine diphosphate | Ligand Info | |||||
| Structure Description | SRPK1 bound to 9mer docking motif peptide | PDB:1WBP | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | No | [5] |
| PDB Sequence |
YHLVKIGDLF
76 NGRYHVIRKL86 GWGHFSTVWL96 SWDIQGKKFV106 AMKVVKSAEH116 YTETALDEIR 126 LLKSVRNSDP136 NDPNREMVVQ146 LLDDFKISGV156 NGTHICMVFE166 VLGHHLLKWI 176 IKSNYQGLPL186 PCVKKIIQQV196 LQGLDYLHTK206 CRIIHTDIKP216 ENILLSVNEQ 226 YIRRLAAEAT236 ENFLVNPLEP485 KNAEKLKVKI495 ADLGNACWVH505 KHFTEDIQTR 515 QYRSLEVLIG525 SGYNTPADIW535 STACMAFELA545 TGDYLFEPHS555 GEEYTRDEDH 565 IALIIELLGK575 VPRKLIVAGK585 YSKEFFTKKG595 DLKHITKLKP605 WGLFEVLVEK 615 YEWSQEEAAG625 FTDFLLPMLE635 LIPEKRATAA645 ECLRHPWLNS655 |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ADP or .ADP2 or .ADP3 or :3ADP;style chemicals stick;color identity;select .A:86 or .A:87 or .A:88 or .A:89 or .A:90 or .A:91 or .A:92 or .A:94 or .A:107 or .A:109 or .A:165 or .A:166 or .A:167 or .A:168 or .A:497; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: AMP-PNP | Ligand Info | |||||
| Structure Description | Crystal structure of SR protein kinase 1 complexed to its substrate ASF/SF2 | PDB:3BEG | ||||
| Method | X-ray diffraction | Resolution | 2.90 Å | Mutation | No | [1] |
| PDB Sequence |
LVKIGDLFNG
78 RYHVIRKLGW88 GHFSTVWLSW98 DIQGKKFVAM108 KVVKSAEHYT118 ETALDEIRLL 128 KSVRNSDPND138 PNREMVVQLL148 DDFKISGVNG158 THICMVFEVL168 GHHLLKWIIK 178 SNYQGLPLPC188 VKKIIQQVLQ198 GLDYLHTKCR208 IIHTDIKPEN218 ILLSVNEQYI 228 RRLAAEAAGN477 FLVNPLEPKN487 AEKLKVKIAD497 LGNACWVHKH507 FTEDIQTRQY 517 RSLEVLIGSG527 YNTPADIWST537 ACMAFELATG547 DYLFEPHSGE557 EYTRDEDHIA 567 LIIELLGKVP577 RKLIVAGKYS587 KEFFTKKGDL597 KHITKLKPWG607 LFEVLVEKYE 617 WSQEEAAGFT627 DFLLPMLELI637 PEKRATAAEC647 LRHPWLNS
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .ANP or .ANP2 or .ANP3 or :3ANP;style chemicals stick;color identity;select .A:86 or .A:87 or .A:88 or .A:89 or .A:90 or .A:91 or .A:92 or .A:94 or .A:107 or .A:109 or .A:165 or .A:166 or .A:167 or .A:168 or .A:171 or .A:220 or .A:497; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: L-serine-O-phosphate | Ligand Info | |||||
| Structure Description | Crystal structure of SR protein kinase 1 complexed to its substrate ASF/SF2 | PDB:3BEG | ||||
| Method | X-ray diffraction | Resolution | 2.90 Å | Mutation | No | [1] |
| PDB Sequence |
LVKIGDLFNG
78 RYHVIRKLGW88 GHFSTVWLSW98 DIQGKKFVAM108 KVVKSAEHYT118 ETALDEIRLL 128 KSVRNSDPND138 PNREMVVQLL148 DDFKISGVNG158 THICMVFEVL168 GHHLLKWIIK 178 SNYQGLPLPC188 VKKIIQQVLQ198 GLDYLHTKCR208 IIHTDIKPEN218 ILLSVNEQYI 228 RRLAAEAAGN477 FLVNPLEPKN487 AEKLKVKIAD497 LGNACWVHKH507 FTEDIQTRQY 517 RSLEVLIGSG527 YNTPADIWST537 ACMAFELATG547 DYLFEPHSGE557 EYTRDEDHIA 567 LIIELLGKVP577 RKLIVAGKYS587 KEFFTKKGDL597 KHITKLKPWG607 LFEVLVEKYE 617 WSQEEAAGFT627 DFLLPMLELI637 PEKRATAAEC647 LRHPWLNS
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .SEP or .SEP2 or .SEP3 or :3SEP;style chemicals stick;color identity;select .A:515 or .A:518 or .A:561; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: 5-Methyl-~{n}-[2-(4-Methylpiperazin-1-Yl)-5-(Trifluoromethyl)phenyl]furan-2-Carboxamide | Ligand Info | |||||
| Structure Description | Crystal structure of human SR protein kinase 1 (SRPK1) in complex with compound 1 | PDB:5MXX | ||||
| Method | X-ray diffraction | Resolution | 1.75 Å | Mutation | No | [3] |
| PDB Sequence |
QEDPNDYCKG
65 GYHLVKIGDL75 FNGRYHVIRK85 LGWGHFSTVW95 LSWDIQGKKF105 VAMKVVKSAE 115 HYTETALDEI125 RLLKSVRNSD135 PNDPNREMVV145 QLLDDFKISG155 VNGTHICMVF 165 EVLGHHLLKW175 IIKSNYQGLP185 LPCVKKIIQQ195 VLQGLDYLHT205 KCRITHTDIK 215 PENILLSVNE225 QYIRRLAAEA235 TENFLVNPLE484 PKNAEKLKVK494 IADLGNACWV 504 HKHFTEDIQT514 RQYRSLEVLI524 GSGYNTPADI534 WSTACMAFEL544 ATGDYLFEPH 554 SGEEYTRDED564 HIALIIELLG574 KVPRKLIVAG584 KYSKEFFTKK594 GDLKHITKLK 604 PWGLFEVLVE614 KYEWSQEEAA624 GFTDFLLPML634 ELIPEKRATA644 AECLRHPWLN 654 S
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .W4A or .W4A2 or .W4A3 or :3W4A;style chemicals stick;color identity;select .A:86 or .A:87 or .A:88 or .A:94 or .A:107 or .A:109 or .A:165 or .A:166 or .A:167 or .A:168 or .A:169 or .A:170 or .A:171 or .A:220 or .A:223 or .A:227 or .A:228 or .A:231; color #f3c393; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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| Ligand Name: N-[3-[[[2-(5-chloro-4-fluoro-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]pyridin-2-yl]-N-methylmethanesulfonamide | Ligand Info | |||||
| Structure Description | SRPK1 in complex with MSC2711186 | PDB:7PQS | ||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [6] |
| PDB Sequence |
GYHLVKIGDL
75 FNGRYHVIRK85 LGWGFSTVWL96 SWDIQGKKFV106 AMKVVKSAEH116 YTETALDEIR 126 LLKSVRNSDP136 NDPNREMVVQ146 LLDDFKISGV156 NGTHICMVFE166 VLGHHLLKWI 176 IKSNYQGLPL186 PCVKKIIQQV196 LQGLDYLHTK206 CRIIHTDIKP216 ENILLSVNEQ 226 YIRRLAAEAT236 EWNFLVNPLE267 PKNAEKLKVK277 IADLGNACWV287 HKHFTEDIQT 297 RQYRSLEVLI307 GSGYNTPADI317 WSTACMAFEL327 ATGDYLFEPH337 SGEEYTRDED 347 HIALIIELLG357 KVPRKLIVAG367 KYSKEFFTKK377 GDLKHITKLK387 PWGLFEVLVE 397 KYEWSQEEAA407 GFTDFLLPML417 ELIPEKRATA427 AECLRHPWLN437 S |
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Click to Show 3D Structure of This Binding Site
set background white;style ions nothing; color 8e8e8e;style chemicals nothing; select .80H or .80H2 or .80H3 or :380H;style chemicals stick;color identity;select .A:86 or .A:87 or .A:88 or .A:89 or .A:92 or .A:94 or .A:107 or .A:109 or .A:145 or .A:165 or .A:166 or .A:167 or .A:168 or .A:169 or .A:170 or .A:171 or .A:174 or .A:217 or .A:218 or .A:220 or .A:223 or .A:227 or .A:231 or .A:279 or .A:280; color #00ffc7; zoom selection;set surface opacity 0.5;set surface Van der Waals surface;set mode all
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LEU86
3.800
GLY87
3.369
TRP88
3.422
GLY89
3.526
SER92
4.337
VAL94
3.483
ALA107
3.674
LYS109
4.539
VAL145
4.462
PHE165
3.666
GLU166
3.255
VAL167
3.133
LEU168
3.163
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | A sliding docking interaction is essential for sequential and processive phosphorylation of an SR protein by SRPK1. Mol Cell. 2008 Mar 14;29(5):563-76. | ||||
| REF 2 | SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform. Cell Chem Biol. 2018 Apr 19;25(4):460-470.e6. | ||||
| REF 3 | Development of Potent, Selective SRPK1 Inhibitors as Potential Topical Therapeutics for Neovascular Eye Disease. ACS Chem Biol. 2017 Mar 17;12(3):825-832. | ||||
| REF 4 | Identification of a Dual Inhibitor of SRPK1 and CK2 That Attenuates Pathological Angiogenesis of Macular Degeneration in Mice. Mol Pharmacol. 2015 Aug;88(2):316-25. | ||||
| REF 5 | Interplay between SRPK and Clk/Sty kinases in phosphorylation of the splicing factor ASF/SF2 is regulated by a docking motif in ASF/SF2. Mol Cell. 2005 Oct 7;20(1):77-89. | ||||
| REF 6 | SRPK1 in complex with MSC2711186 | ||||
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